Hydrogen Or Additional Carbon Bonded Directly To The -c(=x)- Group (e.g., Aldehydes,ketones, Etc.) Patents (Class 548/493)
  • Patent number: 9040709
    Abstract: The present invention relates to a novel method for producing a pyridazinone compound and an intermediate thereof as shown in the following scheme: wherein the symbols are as defined in the specification.
    Type: Grant
    Filed: September 11, 2014
    Date of Patent: May 26, 2015
    Assignee: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Markus Jachmann, Takayuki Wakamatsu, Mitsuharu Anryu
  • Patent number: 9034895
    Abstract: The disclosure provides methods of treating glioblastoma, methods of screening for compounds that treat glioblastoma, and pharmaceutical compositions useful the treatment of glioblastoma.
    Type: Grant
    Filed: August 22, 2011
    Date of Patent: May 19, 2015
    Assignee: University of Washington Through its Center for Commercialization
    Inventors: Nephi Stella, Toni Kline
  • Patent number: 9023871
    Abstract: The present invention provides materials and methods to induce cell death by methuosis, a non-apoptotic cell death mechanism, to induce vacuolization without cell death, or to induce cell death without vacuolization. Small molecules herein are useful for treating cell proliferation disorders or anomalies, particularly, but not exclusively, cancer. Methods related to the research and pharmaceutical use of the small molecules are also provided herein.
    Type: Grant
    Filed: April 7, 2014
    Date of Patent: May 5, 2015
    Assignee: The University of Toledo
    Inventors: William A. Maltese, Paul W. Erhardt, Christopher Trabbic, Jean H. Overmeyer
  • Patent number: 9018394
    Abstract: The invention is a method for efficiently producing an aromatic compound by an intramolecular cyclization reaction, the aromatic compound having a ring structure that includes a nitrogen atom or oxygen atom. An aromatic compound composed of tert-butyl-2-(3-oxo-3-phenylpropyl)phenyl carbamate or another aniline derivative or the like, or an aromatic compound composed of 3-(1-hydroxynaphthalene-2-yl)propionic acid or another naphthol derivative or the like is made to react in a system to which an oxidizing agent and a quaternary ammonium salt represented by general formula (1) are fed. In the formula, X is an iodine atom; and R1, R2, R3 and R4 are each independently a C1-30 hydrocarbon group in which some hydrogen atoms are optionally substituted with halogen atoms, or R1 and R2 may be combine to form a divalent organic group bonded to a nitrogen atom, and R3 and R4 may combine to form a divalent organic group bonded to a nitrogen atom.
    Type: Grant
    Filed: February 2, 2012
    Date of Patent: April 28, 2015
    Assignee: National University Corporation Nagoya University
    Inventors: Kazuaki Ishihara, Uyanik Muhammet
  • Publication number: 20150044293
    Abstract: Radioprotector compounds including 3,3?-diindolylmethane (DIM) analogs, are provided. Further provided are methods for their use in reducing or preventing radiation damage, killing a tumor cell and protecting a non-tumor cell, and treating cancer.
    Type: Application
    Filed: March 14, 2013
    Publication date: February 12, 2015
    Applicant: Georgetown University
    Inventors: Eliot M. Rosen, Milton Brown, Saijun Fan, Thomas Walls, Kathryn E. Ditmer
  • Publication number: 20150045396
    Abstract: The present invention provides a prophylactic or therapeutic agent for giant cell tumors occurring in a bone and soft tissue or for chondrosarcoma, which comprises a non-steroidal anti-inflammatory agent or thiazolidine derivative as an active ingredient, and the like
    Type: Application
    Filed: March 18, 2013
    Publication date: February 12, 2015
    Applicant: NIPPON CHEMIPHAR CO., LTD.
    Inventors: Akihiko Takeuchi, Hiroyuki Tsuchiya
  • Publication number: 20140378688
    Abstract: The present invention relates to a novel method for producing a pyridazinone compound and an intermediate thereof as shown in the following scheme: wherein the symbols are as defined in the specification.
    Type: Application
    Filed: September 11, 2014
    Publication date: December 25, 2014
    Inventors: Markus JACHMANN, Takayuki WAKAMATSU, Mitsuharu ANRYU
  • Patent number: 8884020
    Abstract: Indole derivatives that are useful for treating pain, inflammation and other conditions are described. Certain of the compounds are benzyl derivatives and others are benzoyl derivatives. The compounds are substituted at least at the 3 position of the indole.
    Type: Grant
    Filed: August 7, 2007
    Date of Patent: November 11, 2014
    Assignee: Ironwood Pharmaceuticals, Inc.
    Inventors: John Jeffrey Talley, Kevin Sprott, James Philip Pearson, G. Todd Milne, Wayne Schairer, Jane Yang, Charles Kim, Timothy Barden, Regina Lundrigan, Ara Mermerian, Mark G. Currie
  • Patent number: 8853254
    Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
    Type: Grant
    Filed: October 16, 2012
    Date of Patent: October 7, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara Hadida Ruah, Anna Hazlewood
  • Publication number: 20140213615
    Abstract: The present invention provides materials and methods to induce cell death by methuosis, a non-apoptotic cell death mechanism, to induce vacuolization without cell death, or to induce cell death without vacuolization. Small molecules herein are useful for treating cell proliferation disorders or anomalies, particularly, but not exclusively, cancer. Methods related to the research and pharmaceutical use of the small molecules are also provided herein.
    Type: Application
    Filed: April 7, 2014
    Publication date: July 31, 2014
    Applicant: THE UNIVERSITY OF TOLEDO
    Inventors: William A. Maltese, Paul W. Erhardt, Christopher Trabbic, Jean H. Overmeyer
  • Patent number: 8748411
    Abstract: Chemical compounds derived by in silico molecular modelling, having a well defined structure suitable for the blocking of the phosphorylation event, through the specific interaction of the chemical with the Casein Kinase 2 enzyme substrate phosphorylation domain or it's neighbourhood. This invention comprises also the pharmaceutical compositions containing such compounds, and their use in the preparation of medicines or agents for the treatment of diseases or conditions related with neoplasic processes.
    Type: Grant
    Filed: May 5, 2006
    Date of Patent: June 10, 2014
    Assignee: Centro de Ingenieria Genetica y Biotechnologia
    Inventors: Rolando Eduardo Rodriguez Fernandez, Roberto Vera Alvarez, Ania De La Nuez Veulens, Yuliet Mazola Reyes, Silvio Ernesto Perea Rodriguez, Boris Ernesto Acevedo Castro, Alexis Musacchio Lasa, Raimundo Ubieta Gómez
  • Publication number: 20140155626
    Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
    Type: Application
    Filed: November 18, 2013
    Publication date: June 5, 2014
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Sara Hadida Ruah, Anna Hazlewood, Peter Grootenhuis, Jinglan Zhou
  • Publication number: 20130338371
    Abstract: The invention is a method for efficiently producing an aromatic compound by an intramolecular cyclization reaction, the aromatic compound having a ring structure that includes a nitrogen atom or oxygen atom. An aromatic compound composed of tert-butyl-2-(3-oxo-3-phenylpropyl)phenyl carbamate or another aniline derivative or the like, or an aromatic compound composed of 3-(1-hydroxynaphthalene-2-yl)propionic acid or another naphthol derivative or the like is made to react in a system to which an oxidizing agent and a quaternary ammonium salt represented by general formula (1) are fed. In the formula, X is an iodine atom; and R1, R2, R3 and R4 are each independently a C1-30 hydrocarbon group in which some hydrogen atoms are optionally substituted with halogen atoms, or R1 and R2 may be combine to form a divalent organic group bonded to a nitrogen atom, and R3 and R4 may combine to form a divalent organic group bonded to a nitrogen atom.
    Type: Application
    Filed: February 2, 2012
    Publication date: December 19, 2013
    Applicant: National University Corporation Nagoya University
    Inventors: Kazuaki Ishihara, Uyanik Muhammet
  • Patent number: 8603531
    Abstract: The present invention describes nanoprodrugs of non-steroidal anti-inflammatory drug (NSAIDs) and nanoprodrugs of ?-lipoic acid-containing and NSAIDs. These nanoprodrugs have antioxidant properties and stimuli-responsiveness, which can be used to treat various disease conditions.
    Type: Grant
    Filed: April 8, 2009
    Date of Patent: December 10, 2013
    Assignee: Cedars-Sinai Medical Center
    Inventors: John S. Yu, Bong Seop Lee
  • Publication number: 20130197026
    Abstract: The disclosure provides methods of treating glioblastoma, methods of screening for compounds that treat glioblastoma, and pharmaceutical compositions useful the treatment of glioblastoma.
    Type: Application
    Filed: August 22, 2011
    Publication date: August 1, 2013
    Applicant: Unversity of Washington Through its Center for Commercialization
    Inventors: Nephi Stella, Toni Kline
  • Publication number: 20130172556
    Abstract: The present invention relates to a novel method for producing a pyridazinone compound and an intermediate thereof as shown in the following scheme: wherein the symbols are as defined in the specification.
    Type: Application
    Filed: September 7, 2011
    Publication date: July 4, 2013
    Inventors: Markus Jachmann, Takayuki Wakamatsu, Mitsuharu Anryu
  • Publication number: 20130053315
    Abstract: Novel polypeptide derivatives having protracted profile of action.
    Type: Application
    Filed: March 22, 2012
    Publication date: February 28, 2013
    Inventors: Jesper Lau, Thomas Kruse Hansen, Kjeld Madsen, Paw Bloch, Florencio Zaragoza Dorwald, Nils Langeland Johansen
  • Patent number: 8367665
    Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, carbamate, solvate or salt thereof, including a salt of such an ester, amide or carbamate, and a solvate of such an ester, amide, carbamate or salt. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity, wherein R1, R2, R3, R4, R5 and R6 are as defined in the specification.
    Type: Grant
    Filed: April 16, 2009
    Date of Patent: February 5, 2013
    Assignee: Karo Bio AB
    Inventors: Patrik Rhönnstad, Elisabet Kallin, Theresa Apelqvist, Mattias Wennerstål, Aiping Cheng
  • Patent number: 8314256
    Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
    Type: Grant
    Filed: October 6, 2006
    Date of Patent: November 20, 2012
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara Hadida Ruah, Anna Hazlewood
  • Patent number: 8293895
    Abstract: The present invention relates to novel carbapenem derivatives and belongs to pharmaceutical field. Specifically, the present invention relates to the compounds as represented by formula (1), pharmaceutically acceptable salts, hydrolysable esters, isomers and intermediates thereof, wherein R1, R2, R3, R4 are described as in the description. The present invention also relates to the processes for the preparation of these compounds, to the pharmaceutical compositions comprising these compounds, and to their use for the manufacture of a medicament for the treatment and/or prevention of infectious diseases.
    Type: Grant
    Filed: June 26, 2008
    Date of Patent: October 23, 2012
    Assignee: KBP Biosciences Co., Ltd.
    Inventors: Zhenhua Huang, Yanyan Dong
  • Patent number: 8232310
    Abstract: Peptides and compounds are provided that function as EWS-FLI1 protein inhibitors. The peptides and compounds have utility in the treatment of Ewing's sarcoma family of tumors. Also provided are methods of preparing the compounds and assays for identifying inhibitors of EWS-FLI1 protein.
    Type: Grant
    Filed: June 29, 2009
    Date of Patent: July 31, 2012
    Assignee: Georgetown University
    Inventors: Jeffrey A. Toretsky, Aykut Üren, Milton Lang Brown, Yali Kong
  • Publication number: 20120122942
    Abstract: The present invention relates to novel pharmaceutically-useful compounds which are antagonists of the 5-oxo-ETE receptors, such as the OXE receptor. These compounds have use as therapeutic and/or prophylactic agents for diseases characterized by tissue eosinophilia, such as inflammatory conditions including respiratory diseases. The invention also relates to pharmaceutical compositions, to the use of such compounds and compositions as medicaments, and to therapeutic methods.
    Type: Application
    Filed: May 4, 2010
    Publication date: May 17, 2012
    Inventors: William S. Powell, Joshua Rokach
  • Publication number: 20120040974
    Abstract: The invention provides novel heterocyclic compounds, pharmaceutical compositions and methods of treatment that modulate levels of MIF expression and treat disorders associated with high or low levels of MIF expression.
    Type: Application
    Filed: August 18, 2009
    Publication date: February 16, 2012
    Applicant: YALE UNIVERSITY
    Inventors: William L. Jorgensen, Richard J. Bucala
  • Publication number: 20120034270
    Abstract: The invention relates to novel compounds that have S1P receptor modulating activity and, preferably, apoptotic activity and/or anti proliferative activity against cancer cells and other cell types. Further, the invention relates to a pharmaceutical comprising at least one compound of the invention for the treatment of diseases and/or conditions caused by or associated with in-appropriate S1P receptor modulating activity or expression, for example, cancer. A further aspect of the invention relates to the use of a pharmaceutical comprising at least one compound of the invention for the manufacture of a medicament for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression such as cancer.
    Type: Application
    Filed: October 16, 2009
    Publication date: February 9, 2012
    Applicant: Akaal Pharma Pty Ltd
    Inventors: Damian W. Grobelny, Gurmit S. Gill
  • Publication number: 20110286922
    Abstract: The present invention relates to in vivo imaging and radiotherapeutic methods and agents which target the enzyme aldehyde dehydrogenase (ALDH) and that are suitable for the in vivo imaging of tumours and treatment of cancer.
    Type: Application
    Filed: October 20, 2009
    Publication date: November 24, 2011
    Inventors: Alan Cuthbertson, Peter Brian Iveson, Rajiv Bhalla, Vijaya Raj Kuniyil Kulangara
  • Publication number: 20110190294
    Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, carbamate, solvate or salt thereof, including a salt of such an ester, amide or carbamate, and a solvate of such an ester, amide, carbamate or salt. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity, wherein R1, R2, R3, R4, R5 and R6 are as defined in the specification.
    Type: Application
    Filed: April 16, 2009
    Publication date: August 4, 2011
    Inventors: Patrik Rhönnstad, Elisabet Kallin, Theresa Apelqvist, Mattias Wennerstål, Aiping Cheng
  • Patent number: 7960558
    Abstract: The compounds of the general Formula (I), wherein R1 is aryl or alkyl; R2 represents alkyl; R3 represents alkyl or aralkyl, are valuable pharmaceutical intermediates, which can be prepared by reacting a compound of the general Formula (IV) (wherein the definitions of R1 and R2 are as above), with at least 2 molar equivalents of the compound of the general Formula (VI) (wherein X represents halogen or tertiary butyloxycarbonyloxy group and R3 is as defined above). The known compounds of the general Formula (II) (wherein R1 and R2 are as defined above) are prepared by reacting the compounds of the general Formula (I) with thionyl chloride. The compounds of the general Formula (I) are new intermediates useful in the synthesis of pharmaceutically active ingredients, particularly in the preparation of ACE-inhibitors, e.g. enalapril, perindopril or ramipril.
    Type: Grant
    Filed: May 11, 2007
    Date of Patent: June 14, 2011
    Assignee: Egis Gyogyszergyar Nyilvanosan Mukodo Reszvenytarsasag
    Inventors: Márta Porcs-Makkay, Gyula Simig, Tibor Mezei, Angéla Veressné Pandur, Gyula Lukács
  • Publication number: 20110065685
    Abstract: The present invention provides novel compounds of Formula (I) which are CB2 selective ligands useful for the treatment of pain.
    Type: Application
    Filed: June 14, 2010
    Publication date: March 17, 2011
    Applicant: Abbott Laboratories
    Inventors: Jennifer M. Frost, Karin Tietje, Michael J. Dart, Michael D. Meyer
  • Publication number: 20110039808
    Abstract: There is a need for pharmaceutical compounds which have activity at, at least one of a PPAR and a cannabinoid receptor. Thus there are provided such compounds, wherein the compound comprises: a PPAR pharmacophore and a cannabinoid pharmacophore linked together by a moiety comprising a fused bicyclic ring comprising a five membered ring fused with a six membered ring or a six membered ring fused with a six membered ring; wherein the cannabinoid pharmacophore comprises the fused bicyclic ring; and the PPAR pharmacophore comprises a salicylic acid, alkoxybenzylacetic acid or a alkoxyphenylacetic acid functionality; and wherein the PPAR pharmacophore is linked to the bicyclic ring of the cannabinoid pharmacophore through a linker comprising an amine or an amide functional group.
    Type: Application
    Filed: December 22, 2008
    Publication date: February 17, 2011
    Inventors: Pierre Desreumaux, Salvatore Bellinvia, Philippe Chavatte, Sergio Baroni
  • Patent number: 7858811
    Abstract: A process for the preparation of indoles, e.g. 1,2,3,9-tetrahydro-carbazol-4-one and derivatives thereof.
    Type: Grant
    Filed: November 14, 2006
    Date of Patent: December 28, 2010
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Bernhard Knipp, Ralf Kucznierz, Tim Sattelkau, Thomas Zeibig
  • Publication number: 20100317863
    Abstract: Compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, and R7 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
    Type: Application
    Filed: July 21, 2008
    Publication date: December 16, 2010
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Daniel Kuzmich, John Robinson Regan
  • Patent number: 7846961
    Abstract: ?-crystalline form of the compound of formula (I): characterized by its powder X-ray diffraction diagram. Medicinal products containing the same which are useful as inhibitors of angiotensin I converting enzyme.
    Type: Grant
    Filed: February 26, 2007
    Date of Patent: December 7, 2010
    Assignee: Les Laboratoires Servier
    Inventors: Gérard Coquerel, Loïc Lefebvre, Jean-Claude Souvie, Pascale Authouart
  • Publication number: 20100292157
    Abstract: The invention relates generally to novel compositions and methods comprising a cyclohexanehexol and a secretase inhibitor. The compositions and methods provide beneficial effects, in particular sustained beneficial effects, in the treatment of diseases involving a disorder in protein folding and/or aggregation, and/or amyloid formation, deposition, accumulation, or persistence, such as Alzheimer's disease and related neurodegenerative disorders.
    Type: Application
    Filed: November 22, 2007
    Publication date: November 18, 2010
    Inventor: Antonio Cruz
  • Publication number: 20100286404
    Abstract: The compounds of the general Formula (I), wherein R1 is aryl or alkyl; R2 represents alkyl; R3 represents alkyl or aralkyl, are valuable pharmaceutical intermediates, which can be prepared by reacting a compound of the general Formula (IV) (wherein the definitions of R1 and R2 are as above), with at least 2 molar equivalents of the compound of the general Formula (VI) (wherein X represents halogen or tertiary butyloxycarbonyloxy group and R3 is as defined above). The known compounds of the general Formula (II) (wherein R1 and R2 are as defined above) are prepared by reacting the compounds of the general Formula (I) with thionyl chloride. The compounds of the general Formula (I) are new intermediates useful in the synthesis of pharmaceutically active ingredients, particularly in the preparation of ACE-inhibitors, e.g. enalapril, perindopril or ramipril.
    Type: Application
    Filed: May 11, 2007
    Publication date: November 11, 2010
    Inventors: Marta Porcs-Makkay, Gyula Simig, Tibor Mezei, Angéla Veressné Pandur, Gyula Lukács
  • Publication number: 20100286144
    Abstract: A compound of the following formula (1), or its prodrug or pharmaceutically acceptable salt thereof, being useful as a diabetic medicine or preventive, or blood sugar regulator, or therapeutic agent for hyperlipemia, etc. wherein the ring Z is an optionally substituted heteroaryl, W4 is a single bond, lower alkylene, etc., Ar2 is an optionally substituted aryl, etc., W3 is a single bond, lower alkylene, etc., Ar1 is an optionally substituted arylene, etc., each of W1 and W2 is an optionally substituted lower alkylene, etc., and R1 is carboxyl, an alkoxycarbonyl.
    Type: Application
    Filed: July 21, 2010
    Publication date: November 11, 2010
    Inventors: Yoko TAKAHASHI, Ryu Nagata, Kantaro Ushiroda
  • Publication number: 20100240718
    Abstract: The present invention relates to novel heteroaryl-substituted acetone derivatives inhibiting the enzyme phospholipase A2, and pharmaceutical agents comprising said compounds.
    Type: Application
    Filed: September 19, 2008
    Publication date: September 23, 2010
    Applicant: WESTFALISCHE WILHELMS UNIVERSITÄT MÜNSTER
    Inventors: Matthias Lehr, Stefanie Bovens
  • Patent number: 7781479
    Abstract: A compound of the following formula (1), or its prodrug or pharmaceutically acceptable salt thereof, being useful as a diabetic medicine or preventive, or blood sugar regulator, or therapeutic agent for hyperlipemia, etc. wherein the ring Z is an optionally substituted heteroaryl, W4 is a single bond, lower alkylene, etc., Ar2 is an optionally substituted aryl, etc., W3 is a single bond, lower alkylene, etc., Ar1 is an optionally substituted arylene, etc., each of W1 and W2 is an optionally substituted lower alkylene, etc., and R1 is carboxyl, an alkoxycarbonyl.
    Type: Grant
    Filed: January 12, 2006
    Date of Patent: August 24, 2010
    Assignee: Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Yoko Takahashi, Ryu Nagata, Kantaro Ushiroda
  • Patent number: 7772216
    Abstract: The present invention provides a method for identifying inhibitors of protein kinases and/or protein phosphatases. Methods are also provided for inhibiting protein kinase and/or protein phosphatase activity. Specific non-peptide protein tyrosine kinase and/or protein phosphatase inhibitors are provided. The protein kinase or protein phosphatase inhibitors of the present invention may be used to treat a number of conditions in patients, including cancer, psoriasis, arthrosclerosis, immune system activity, Type II diabetes, and obesity.
    Type: Grant
    Filed: August 16, 2005
    Date of Patent: August 10, 2010
    Assignee: The Research Foundation of State University of New York
    Inventors: David G. Hangauer, Jr., Moustafa E. El-Araby, Karen L. Milkiewicz
  • Publication number: 20100197938
    Abstract: There is provided a novel process for producing an indole derivative which comprises cyclizing 2-nitrobenzylcarbony compound in the presence of a catalyst comprising a Group VIII metal of the Periodic Table, characterized by conducting the cyclization in a gas atmosphere containing carbon monoxide. The process enables an indole compound to be selectively produced in a high yield from 2-nitrobenzylcarbonyl compound, and hardly yields an indoline compound as a reduction by-product that has been a problem in the catalytic hydrogenation method employing a noble metal catalyst. The indole derivative produced by the present process is useful for various fine chemical intermediates including compounds and physiologically active substances such as pharmaceuticals and agrochemicals.
    Type: Application
    Filed: April 2, 2010
    Publication date: August 5, 2010
    Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.
    Inventors: Yasuhiro Sakurai, Tomohisa Utsunomiya, Norio Tanaka
  • Publication number: 20100197708
    Abstract: Indole derivatives that are useful for treating pain, inflammation and other conditions are described. Certain of the compounds are benzyl derivatives and others are benzoyl derivatives. The compounds are substituted at least at the 3 position of the indole.
    Type: Application
    Filed: August 7, 2007
    Publication date: August 5, 2010
    Inventors: John Jeffrey Talley, Kevin Sprott, James Philip Pearson, G. Todd Milne, Wayne Schairer, Jane Yang, Charles Kim, Timothy Barden, Regina Lundrigan, Ara Mermerian, Mark G. Currie
  • Patent number: 7741363
    Abstract: The invention relates to compounds of formula (I), wherein X, R1, R2, R3, R4 and R5 are as described herein. The invention also includes preparative methods for the preparation of compounds of formula (I). A method for the therapeutic use of the inventive compounds is also disclosed and claimed.
    Type: Grant
    Filed: May 14, 2008
    Date of Patent: June 22, 2010
    Assignee: Sanofi-Aventis
    Inventors: Francis Barth, Claude Vernhet, Murielle Rinaldi-Carmona, CaroleElisabeth Guillaumont-Legeay
  • Publication number: 20100137291
    Abstract: The invention describes novel nitrosated nonsteroidal antiinflammatory drugs (NSAIDs) and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated NSAID, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one nitrosated NSAID, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one nitrosated NSAID, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent.
    Type: Application
    Filed: December 11, 2009
    Publication date: June 3, 2010
    Inventors: Richard A. EARL, Maiko EZAWA, Xinqin FANG, David S. GARVEY, Ricky D. GASTON, Subhash P. KHANAPURE, L. Gordon LETTS, Chia-En LIN, Ramani R. RANATUNGA, Stewart K. RICHARDSON, Joseph D. SCHROEDER, Cheri A. STEVENSON, Shiow-Jyi WEY
  • Publication number: 20100113777
    Abstract: A compound, or its salt, or a solvate thereof having a cPLA2 inhibiting activity having the formula (I): or a pharmaceutical composition, cPLA2 inhibitor and inhibitors of various lipid mediator production containing the same as active ingredients.
    Type: Application
    Filed: March 28, 2008
    Publication date: May 6, 2010
    Applicant: Asubio Pharma Co., Ltd.
    Inventors: Toshiyuki Tomoo, Takashi Nakatsuka, Yasuhiro Hayashi, Toyoko Katayama
  • Patent number: 7683092
    Abstract: Novel crystalline forms of two indole compounds connected to phenoxyalkylcarboxylic acid groups are selective PPAR gamma partial agonists that are useful in the treatment of type 2 diabetes, hyperglycemia, obesity, dyslipidemia, and the metabolic syndrome. The novel crystal forms include a crystalline free acid dihydrate and crystalline free acid anhydrate of one compound and several crystalline forms of the free acid and the sodium salt of the second compound. The invention also relates to pharmaceutical compositions comprising these novel crystal forms, processes to prepare the crystal forms and their pharmaceutical compositions, and uses of the crystal forms in the treatment of type 2 diabetes and other PPAR gamma modulated diseases.
    Type: Grant
    Filed: March 10, 2006
    Date of Patent: March 23, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Dalian Zhao, Jean-Francois Marcoux, David Boardman, Aquiles E. Leyes
  • Patent number: 7674818
    Abstract: Compounds of formula I are provided: wherein: R1, R2, and R3, are as defined herein, as well as pharmaceutical composition and methods using the compounds as inhibitors of plasminogen activator inhibitor (PAI-1) and as therapeutic composition for treating conditions resulting from fibrinolytic disorders, such as deep vein thrombosis, coronary heart disease and pulmonary fibrosis.
    Type: Grant
    Filed: July 11, 2007
    Date of Patent: March 9, 2010
    Assignee: Wyeth LLC
    Inventors: Lee Dalton Jennings, Hassan Mahmoud Elokdah, Geraldine Ruth McFarlane
  • Patent number: 7598398
    Abstract: The present invention relates to substituted indoles, compositions containing such compounds and methods of treatment The compounds are glucagon receptor antagonists and thus are useful for treating, preventing or delaying the onset of type 2 diabetes mellitus and related conditions.
    Type: Grant
    Filed: October 13, 2006
    Date of Patent: October 6, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Ronald M. Kim, Amy R. Bittner, Christopher Joseph Sinz, Emma R. Parmee
  • Patent number: 7566791
    Abstract: Substituted 3-carbonyl-1H-indol-1-yl acetic acid derivatives of formula I are provided: wherein: R1, R2, R3, R4 and R5 are as defined herein which are useful as inhibitors of plasminogen activator inhibitor-1 (PAI-1) for treating conditions resulting from fibrinolytic disorders, such as deep vein thrombosis and coronary heart disease, and pulmonary fibrosis.
    Type: Grant
    Filed: March 15, 2006
    Date of Patent: July 28, 2009
    Assignee: Wyeth
    Inventor: Lee D. Jennings
  • Publication number: 20090124620
    Abstract: The present invention relates to an inhibitor of plasminogen activator inhibitor-1. The present invention further relates to a pharmaceutical composition that has an inhibitory action on PAI-1 activity and is useful in the prevention and treatment of various diseases whose onset is associated with PAI-1 activity. Furthermore, the present invention relates to a novel compound having PAI-1 inhibitory activity represented by the following general formula (I), and a salt thereof. Each symbol is defined as those in the specification.
    Type: Application
    Filed: March 12, 2008
    Publication date: May 14, 2009
    Inventors: Toshio Miyata, Nagahisa Yamaoka, Hidehiko Kodama
  • Publication number: 20090123555
    Abstract: The invention relates to spherical particles formed by polymer chains containing approximately from 30 to 10000 monomer units derived from monocyclic polycyclic alkene polymerization, wherein at least one monomer unit is substituted by an R chain including ethylene polyoxide which is optionally covalently linked to the polymer units through a hydrolyzable bridge and substituted by a reactive function, optionally engaged in a link with an active principle or a biological molecule such as protein, wherein the chain R is covalently linked to the monomer units. The use of the inventive spherical particles for preparing pharmaceutical and cosmetic compositions or surface coatings is also disclosed.
    Type: Application
    Filed: June 21, 2005
    Publication date: May 14, 2009
    Applicants: CENTRE NATIONAL DE LA RECHER CHE SCIENTIFIQUE, INSERM INSTITUT NATIONAL DE LA SANTE ET DE LA SANT, UNIVERSITE DE BORDEAUX I, ECOLE NATIONALE SUPERIEURE DE CHIMIE ET DE PHYSIQU
    Inventors: Valerie Sabaut-Heroguez, Damien Quemener, Marie-Christine Durrieu
  • Patent number: 7459478
    Abstract: Compounds of formula (I) and II) are provided wherein: X is an alkali metal or a basic amine moiety; R1 is alkyl, cycloalkyl, —CH2-cycloalkyl, pyridinyl, —CH2-pyridinyl, phenyl or benzyl, the rings of these groups being optionally substituted; R2 is H, halogen, alkyl, perfluoroalkyl, alkoxy, cycloalkyl, —CH2-cycloalkyl, —NH2, or —NO2; R3 is phenyl, benzyl, benzyloxy, pyridinyl, or —CH2-pyridinyl, with the rings of these groups being optionally substituted; or a pharmaceutically acceptable salt or ester form thereof, as well as pharmaceutical compositions and methods using these compounds as inhibitors of plasminogen activator inhibitor-1 (PAI-1) and as therapeutic compositions for treating conditions resulting from fibrinolytic disorders such as deep vein thrombosis and coronary heart disease, and pulmonary fibrosis.
    Type: Grant
    Filed: June 5, 2006
    Date of Patent: December 2, 2008
    Assignee: Wyeth
    Inventors: Hassan Mahmound Elokdah, David Zenan Li